CA2352505C - Derives d'epothilone et leur utilisation comme agents antitumoraux - Google Patents

Derives d'epothilone et leur utilisation comme agents antitumoraux Download PDF

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Publication number
CA2352505C
CA2352505C CA002352505A CA2352505A CA2352505C CA 2352505 C CA2352505 C CA 2352505C CA 002352505 A CA002352505 A CA 002352505A CA 2352505 A CA2352505 A CA 2352505A CA 2352505 C CA2352505 C CA 2352505C
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CA
Canada
Prior art keywords
alkyl
formula
compound
salt
bond
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CA002352505A
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English (en)
Other versions
CA2352505A1 (fr
Inventor
Karl-Heinz Altmann
Guido Bold
Giorgio Caravatti
Andreas Florsheimer
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Novartis AG
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Novartis AG
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Filing date
Publication date
Application filed by Novartis AG filed Critical Novartis AG
Publication of CA2352505A1 publication Critical patent/CA2352505A1/fr
Application granted granted Critical
Publication of CA2352505C publication Critical patent/CA2352505C/fr
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Silicon Polymers (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

L'invention concerne des composés antitumoraux efficaces de formule I, dans laquelle les radicaux ont la signification indiquée dans la description.
CA002352505A 1998-12-22 1999-12-20 Derives d'epothilone et leur utilisation comme agents antitumoraux Expired - Fee Related CA2352505C (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CH253098 1998-12-22
CH2530/98 1998-12-22
PCT/EP1999/010129 WO2000037473A1 (fr) 1998-12-22 1999-12-20 Derives d'epothilone et leur utilisation comme agents antitumoraux

Publications (2)

Publication Number Publication Date
CA2352505A1 CA2352505A1 (fr) 2000-06-29
CA2352505C true CA2352505C (fr) 2009-04-07

Family

ID=4235876

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002352505A Expired - Fee Related CA2352505C (fr) 1998-12-22 1999-12-20 Derives d'epothilone et leur utilisation comme agents antitumoraux

Country Status (12)

Country Link
US (1) US6387927B1 (fr)
EP (1) EP1140944B1 (fr)
JP (1) JP2002533346A (fr)
CN (1) CN1122668C (fr)
AT (1) ATE248175T1 (fr)
AU (1) AU2795000A (fr)
BR (1) BR9916833A (fr)
CA (1) CA2352505C (fr)
DE (1) DE69910831T2 (fr)
ES (1) ES2207983T3 (fr)
PT (1) PT1140944E (fr)
WO (1) WO2000037473A1 (fr)

Families Citing this family (68)

* Cited by examiner, † Cited by third party
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ATE218556T1 (de) 1995-11-17 2002-06-15 Biotechnolog Forschung Gmbh Epothilon-derivate und deren herstellung
JP4274583B2 (ja) 1996-11-18 2009-06-10 ゲゼルシャフト・フュア・ビオテクノロギッシェ・フォルシュンク・ミット・ベシュレンクテル・ハフツング（ゲー・ベー・エフ） エポチロンｃ，ｄ，ｅ及びｆ、製造と薬剤
US6242469B1 (en) 1996-12-03 2001-06-05 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US20050043376A1 (en) * 1996-12-03 2005-02-24 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US6204388B1 (en) 1996-12-03 2001-03-20 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US6605599B1 (en) 1997-07-08 2003-08-12 Bristol-Myers Squibb Company Epothilone derivatives
US6365749B1 (en) 1997-12-04 2002-04-02 Bristol-Myers Squibb Company Process for the preparation of ring-opened epothilone intermediates which are useful for the preparation of epothilone analogs
US6498257B1 (en) 1998-04-21 2002-12-24 Bristol-Myers Squibb Company 2,3-olefinic epothilone derivatives
US6380395B1 (en) 1998-04-21 2002-04-30 Bristol-Myers Squibb Company 12, 13-cyclopropane epothilone derivatives
US20020058286A1 (en) * 1999-02-24 2002-05-16 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto and analogues thereof
US6518421B1 (en) * 2000-03-20 2003-02-11 Bristol-Myers Squibb Company Process for the preparation of epothilone analogs
US6593115B2 (en) 2000-03-24 2003-07-15 Bristol-Myers Squibb Co. Preparation of epothilone intermediates
WO2001092255A2 (fr) * 2000-05-26 2001-12-06 Kosan Biosciences, Inc. Derives d'epothilone, procedes de production et methodes d'utilisation
US6448281B1 (en) * 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
UA75365C2 (en) * 2000-08-16 2006-04-17 Bristol Myers Squibb Co Epothilone analog polymorph modifications, a method for obtaining thereof (variants), a pharmaceutical composition based thereon
US20020111317A1 (en) * 2000-09-25 2002-08-15 Leonard Katz Sixteen-membered macrolide compounds
NZ526871A (en) * 2001-01-25 2006-01-27 Bristol Myers Squibb Co Pharmaceutical dosage forms of epothilones for oral administration
CZ20032021A3 (cs) 2001-01-25 2004-05-12 Bristol@Myersásquibbácompany Způsoby podávání analogů epothilonu při léčbě rakoviny
EP1353667A1 (fr) * 2001-01-25 2003-10-22 Bristol-Myers Squibb Company Formulations parenterales contenant des analogues d'epothilone
MXPA03007423A (es) 2001-02-20 2003-11-18 Bristol Myers Squibb Co Derivados de epotilona para tratamiento de tumores refractarios.
WO2002066038A1 (fr) 2001-02-20 2002-08-29 Bristol-Myers Squibb Company Traitement de tumeurs refractaires a l'aide de derives d'epothilone
CA2440555A1 (fr) 2001-03-14 2002-09-19 Bristol-Myers Squibb Company Combinaison d'analogues d'epothilones et d'agents chimiotherapeutiques servant au traitement de maladies proliferatives
SI1372650T1 (sl) * 2001-03-19 2009-04-30 Novartis Ag Kombinacije, ki obsegajo antidiaroično sredstvo in epotilon ali epotilonski derivat
WO2002098868A1 (fr) * 2001-06-01 2002-12-12 Bristol-Myers Squibb Company Derives d'epothilone
WO2003031414A1 (fr) * 2001-10-03 2003-04-17 Nippon Soda Co.,Ltd. Nouveau compose heterocyclique et agent anti-inflammatoire
RU2346686C2 (ru) * 2002-01-14 2009-02-20 Новартис Аг Комбинации, включающие эпотилоны и антиметаболиты
TW200303202A (en) * 2002-02-15 2003-09-01 Bristol Myers Squibb Co Method of preparation of 21-amino epothilone derivatives
WO2003077903A1 (fr) 2002-03-12 2003-09-25 Bristol-Myers Squibb Company Derives c12-cyano epothilone
DK1483251T3 (da) 2002-03-12 2010-04-12 Bristol Myers Squibb Co C3-cyano-epothilon-derivater
TW200403994A (en) 2002-04-04 2004-03-16 Bristol Myers Squibb Co Oral administration of EPOTHILONES
TW200400191A (en) 2002-05-15 2004-01-01 Bristol Myers Squibb Co Pharmaceutical compositions and methods of using C-21 modified epothilone derivatives
US7008936B2 (en) 2002-06-14 2006-03-07 Bristol-Myers Squibb Company Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases
WO2004018478A2 (fr) 2002-08-23 2004-03-04 Sloan-Kettering Institute For Cancer Research Synthese d'epothilones, leurs intermediaires, leurs analogues et leurs utilisations
US6921769B2 (en) 2002-08-23 2005-07-26 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
AR041137A1 (es) 2002-09-04 2005-05-04 Pharmacopeia Drug Discovery Pirazolopirimidinas como inhibidores de quinasa dependientes de ciclinas
GB0221312D0 (en) * 2002-09-13 2002-10-23 Novartis Ag Organic compounds
KR20050053681A (ko) 2002-09-23 2005-06-08 브리스톨-마이어스 스큅 컴퍼니 에포틸론 ｂ의 제조, 분리 및 정제 방법, 및 에포틸론 ｂ의ｘ-선 결정 구조
US7112581B2 (en) 2002-09-27 2006-09-26 Nereus Pharmaceuticals, Inc. Macrocyclic lactams
DE10256982A1 (de) * 2002-12-05 2004-06-24 Schering Ag Neue Effektor-Konjugate, Verfahren zu Ihrer Herstellung und Ihre Pharmazeutische Verwendung
US20040146632A1 (en) * 2003-01-23 2004-07-29 Cristina Sayman Effective multi-component penetrating and flavoring marinade
US20050171167A1 (en) * 2003-11-04 2005-08-04 Haby Thomas A. Process and formulation containing epothilones and analogs thereof
GB0405898D0 (en) * 2004-03-16 2004-04-21 Novartis Ag Organic compounds
US7122700B2 (en) * 2004-07-30 2006-10-17 Xerox Corporation Arylamine processes
EP1640004A1 (fr) * 2004-09-24 2006-03-29 Schering Aktiengesellschaft Utilisation des epothilones pour le traitement des metastases osseuses ou du cancer des os
EP1674098A1 (fr) 2004-12-23 2006-06-28 Schering Aktiengesellschaft Formulations parenterales stables et tolérables des substances de haut réactivité ayant une solubilité basse ou inexistante dans l'eau
JP2008536479A (ja) 2005-02-11 2008-09-11 ユニバーシティ オブ サザン カリフォルニア ジスルフィド架橋を有するタンパク質の発現法
JP4954983B2 (ja) 2005-05-18 2012-06-20 ファーマサイエンス・インコーポレイテッド Ｂｉｒドメイン結合化合物
EP1845096A1 (fr) * 2006-03-27 2007-10-17 ETH Zürich 12-Aza-epothilones, procédé de préparation et leur utilisation comme agents antiproliferatives
US8008256B2 (en) * 2006-05-01 2011-08-30 University Of Southern California Combination therapy for treatment of cancer
SG10201407457UA (en) 2006-05-16 2014-12-30 Pharmascience Inc Iap bir domain binding compounds
DE102007016046A1 (de) * 2007-03-30 2008-10-23 Bayer Schering Pharma Aktiengesellschaft Verfahren zur Herstellung von Epothilonderivaten durch selektive katalytische Epoxidierung
EP2065054A1 (fr) 2007-11-29 2009-06-03 Bayer Schering Pharma Aktiengesellschaft Combinaisons comprenant une prostaglandine et leurs utilisations
EP2070521A1 (fr) 2007-12-10 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Nanoparticules à surface modifiée
DE102007059752A1 (de) 2007-12-10 2009-06-18 Bayer Schering Pharma Aktiengesellschaft Funktionalisierte, feste Polymernanopartikel enthaltend Epothilone
CN101519404B (zh) * 2008-02-29 2016-01-20 唐莉 15环噻酮衍生物及其制备方法与应用
US8802394B2 (en) 2008-11-13 2014-08-12 Radu O. Minea Method of expressing proteins with disulfide bridges with enhanced yields and activity
EP2210584A1 (fr) 2009-01-27 2010-07-28 Bayer Schering Pharma Aktiengesellschaft Composition polymère stable comprenant un copolymère séquencé d'épothilone et amphiphile
MX340870B (es) 2010-02-12 2016-07-27 Pharmascience Inc Compuestos de unión del dominio de repetición de inhibidores de proteínas de apoptosis de baculovirus.
CN103037903A (zh) 2010-05-18 2013-04-10 天蓝制药公司 用于治疗自身免疫性疾病或其它疾病的组合物和方法
AU2012356894B2 (en) 2011-12-23 2018-01-18 Araris Biotech Ltd. Enzymatic conjugation of polypeptides
WO2014009426A2 (fr) 2012-07-13 2014-01-16 Innate Pharma Criblage d'anticorps conjugués
EP2916872B1 (fr) 2012-11-09 2019-02-27 Innate Pharma Etiquettes de reconnaissance pour la conjugaison à médiation par la tgase
WO2014140300A1 (fr) 2013-03-15 2014-09-18 Innate Pharma Conjugaison d'anticorps en phase solide médiée par la tgase
WO2014202773A1 (fr) 2013-06-20 2014-12-24 Innate Pharma Conjugaison enzymatique de polypeptides
JP6744212B2 (ja) 2013-06-21 2020-08-19 イナート・ファルマ・ソシエテ・アノニムＩｎｎａｔｅ Ｐｈａｒｍａ Ｐｈａｒｍａ Ｓ．Ａ． ポリペプチドの酵素的結合
WO2019092148A1 (fr) 2017-11-10 2019-05-16 Innate Pharma Anticorps avec des résidus de glutamine fonctionnalisés

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6242469B1 (en) * 1996-12-03 2001-06-05 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US6605599B1 (en) * 1997-07-08 2003-08-12 Bristol-Myers Squibb Company Epothilone derivatives

Also Published As

Publication number Publication date
BR9916833A (pt) 2001-09-25
CA2352505A1 (fr) 2000-06-29
EP1140944B1 (fr) 2003-08-27
CN1332742A (zh) 2002-01-23
CN1122668C (zh) 2003-10-01
US6387927B1 (en) 2002-05-14
DE69910831T2 (de) 2004-07-15
AU2795000A (en) 2000-07-12
WO2000037473A1 (fr) 2000-06-29
JP2002533346A (ja) 2002-10-08
DE69910831D1 (de) 2003-10-02
EP1140944A1 (fr) 2001-10-10
PT1140944E (pt) 2004-01-30
ES2207983T3 (es) 2004-06-01
ATE248175T1 (de) 2003-09-15

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